(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)(thiophen-2-yl)methanone | 121306-85-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: (5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)(thiophen-2-yl)methanone
• 英文别名: 1-(2-Thienylcarbonyl)-5-phenyl-2-pyrazoline；(3-phenyl-3,4-dihydropyrazol-2-yl)-thiophen-2-ylmethanone
• CAS: 121306-85-2
• 化学式: C₁₄H₁₂N₂OS
• 分子量: 256.328
• InChiKey: XHFCWCMBADMELI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  60.9
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] HETEROCYCLIC AMIDES AS KINASE INHIBITORS<br/>[FR] AMIDES HÉTÉROCYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE KINASE
  申请人：GLAXOSMITHKLINE IP DEV LTD

  公开号：WO2016185423A1

  公开（公告）日：2016-11-24

  Disclosed are compounds having the formula: (I) wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

  揭示的是具有以下式的化合物：(I) 其中R1、R2和R3如本文所定义，并且制备和使用这些化合物的方法。
• Pyrazoline derivatives and agents for treating cerebrovascular diseases containing the same as active ingredient
  申请人：MITSUI TOATSU CHEMICALS, Inc.

  公开号：EP0295695A2

  公开（公告）日：1988-12-21

  This invention relates to new 2-pyrazoline derivatives represented by the following general formula (A): ( wherein R¹ denotes a pyridyl, a pyrazyl or an alkoxyl group; and R² stands for hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group ), and to a process for producing the same. This invention also relates to agents for treating cerebrovascular diseases containing, as active ingredients, a 2-pyrazoline derivative represented by the following general formula (G): ( wherein R³ denotes hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcabonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-sub­stituted thiocarbamoyl, or carboxyl group; and R⁴ stands for hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group ) or a pharmaceutically acceptable salt thereof. Administration of an agent of this invention for treat­ing cerebrovascular diseases copes with cerebral edemata in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial blood circulation, thereby protecting ischemic lesions and minimizing the spread of affected parts.

  本发明涉及由以下通式(A)代表的新的 2-吡唑啉衍生物： (其中，R¹表示吡啶基、吡嗪基或烷氧基；R²表示氢原子、烷基、吡啶基、呋喃基、苯基或取代苯基），并涉及其生产工艺。本发明还涉及治疗脑血管疾病的制剂，其活性成分含有下通式（G）代表的 2-吡唑啉衍生物： (其中 R³ 表示氢原子、烷基、乙酰基、烷氧羰基、氨基、苯甲酰基、取代苯甲酰基、吡啶羰基、呋喃羰基、噻吩羰基、吡嗪羰基、N-取代氨基甲酰基、N-取代硫代氨基甲酰基或羧基；R⁴代表氢原子、烷基、吡啶基、噻吩基、呋喃基、环己基、苯基或取代苯基）或其药学上可接受的盐。 服用本发明治疗脑血管疾病的制剂，可在脑中风的急性期处理脑水肿，调节全身和颅内血液循环，从而保护缺血性病变，最大限度地减少受影响部位的扩散。
• Heterocyclic amides as kinase inhibitors
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：US10590085B2

  公开（公告）日：2020-03-17

  Disclosed are compounds having the formula (I): wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

  公开了具有式 (I) 的化合物： 其中 R1、R2 和 R3 如本文所定义，以及制造和使用它们的方法。
• HETEROCYCLIC AMIDES AS KINASE INHIBITORS
  申请人：GlaxoSmithKline Intellectual Property Development Limited

  公开号：EP3298002A1

  公开（公告）日：2018-03-28
• Heterocyclic Amides as Kinase Inhibitors
  申请人：GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

  公开号：US20210253532A1

  公开（公告）日：2021-08-19

  Disclosed are compounds having the formula: wherein R 1 , R 2 , and R 3 are as defined herein, and methods of making and using the same.